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Synthesis, anti-oomycete activity, and SAR studies of paeonol derivatives
Journal of Asian Natural Products Research ( IF 1.7 ) Pub Date : 2020-02-03 , DOI: 10.1080/10286020.2020.1718116
Yue-E Tian 1 , Di Sun 1 , Xiao-Xiao Han 1 , Jin-Ming Yang 1 , Song Zhang 1 , Nan-Nan Feng 1 , Li-Na Zhu 1 , Zhong-Yuan Xu 1 , Zhi-Ping Che 1 , Sheng-Ming Liu 1 , Xiao-Min Lin 1 , Jia Jiang 1 , Gen-Qiang Chen 1
Affiliation  

Abstract

Three series of sulfonate derivatives of paeonol were synthesized and screened in vitro for their anti-oomycete activity against P. capsici, respectively. Among all the compounds, 4m displayed the best promising and pronounced anti-oomycete activity against P. capsici than zoxamide, with the EC50 values of 24.51 and 26.87 mg/L, respectively. The results show that acetyl and 4-OCH3 are two necessary groups. The existence of these two sites is closely related to the anti-oomycete activity. Relatively speaking, hydroxyl group is well tolerated, and the results showed that after modification of hydroxyl group with sulfonyl, the anti-oomycete activity was significantly increased.



中文翻译:

丹皮酚衍生物的合成,抗卵菌活性和SAR研究

摘要

三个系列丹皮酚磺酸酯衍生物的合成和筛选体外针对它们的抗卵菌纲活性辣椒疫霉,分别。在所有化合物中,4米显示针对最好有为和显着的抗卵菌纲活性辣椒疫霉比苯酰菌胺,与EC 50分别为24.51的值和26.87毫克/ L。结果表明,乙酰基和4-OCH 3是两个必要的基团。这两个位点的存在与抗卵菌活性密切相关。相对而言,羟基具有良好的耐受性,结果表明,用磺酰基修饰羟基后,抗卵菌活性显着提高。

更新日期:2020-02-03
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